Stone T W
Br J Pharmacol. 1985 Jan;84(1):165-73.
Phosphorothioate analogues of adenosine 5'-triphosphate (ATP) have been tested on the rat and guinea-pig vas deferens, the guinea-pig taenia coli and urinary bladder. Adenosine 5'0-(2-thiotriphosphate) (ATP beta S) was more active than adenosine 5'0(1-thiotriphosphate) (ATP alpha S) and ATP in producing contractile responses on the vas deferens of rat and guinea-pig, and guinea-pig bladder, though the difference of potency was less marked for producing relaxation of the carbachol-contracted taenia coli. No differences were observed between the A and B diastereoisomers of ATP alpha S or ATP beta S. Contractions of the vas deferens produced by ATP alpha S were of much longer duration than those produced by ATP beta S. When tested against electrically-evoked twitch responses of the vas deferens the order of potencies was reversed with ATP being most active and ATP beta S least active. These inhibitory effects were blocked by 8-phenyl-theophylline. The calculated pA2 values for ATP, adenosine, beta, gamma-methylene ATP (APPCP) and ATP alpha S were similar, suggesting a common site of action. The results do not reveal any stereoselectivity among the tissues tested, for the diastereoisomers of ATP phosphorothioates; the observed differences of potency may be due to differences between ATP alpha S and ATP beta S in their rates of metabolism to adenosine. The different response profiles to the phosphorothioates may however reflect some differences of receptor mechanisms.
三磷酸腺苷（ATP）的硫代磷酸酯类似物已在大鼠和豚鼠的输精管、豚鼠的结肠带和膀胱上进行了测试。5'-O-(2-硫代三磷酸)腺苷（ATPβS）在对大鼠和豚鼠的输精管以及豚鼠膀胱产生收缩反应方面比5'-O-(1-硫代三磷酸)腺苷（ATPαS）和ATP更具活性，尽管在使卡巴胆碱收缩的结肠带松弛方面效力差异不太明显。在ATPαS或ATPβS的A和B非对映异构体之间未观察到差异。ATPαS引起的输精管收缩持续时间比ATPβS引起的长得多。当针对输精管的电诱发抽搐反应进行测试时，效力顺序相反，ATP最具活性，ATPβS最不具活性。这些抑制作用被8-苯基茶碱阻断。ATP、腺苷、β,γ-亚甲基ATP（APPCP）和ATPαS的计算pA2值相似，表明作用位点相同。结果并未揭示在所测试的组织中，对于ATP硫代磷酸酯的非对映异构体存在任何立体选择性；观察到的效力差异可能是由于ATPαS和ATPβS代谢为腺苷的速率不同。然而，对硫代磷酸酯的不同反应特征可能反映了受体机制的一些差异。
